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CVPR Unit 2 > Anticoagulants and Antiplatelet Drugs > Flashcards

Anticoagulants and Antiplatelet Drugs Flashcards

1
Q

Factor IIa Inhibitors

A

Unfractionated Heparin*
Dabigatran
Fondaparinux

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2
Q

Heparin Site of Action

A

Combines with antithrombin III (ATIII) to inactivate active clotting factors (IIa, IXa, Xa, XIa, XIIa)

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3
Q

LMWHs/ Fondaparinux Site of Action

A

Combine with antithrombin III (ATIII) to inactivate Xa

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4
Q

Hirudin, Dabigatran Site of Action

A

Directly inactivate IIa (thrombin)

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5
Q

Rivaroxaban Site of Action

A

Directly inactivates Xa

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6
Q

Venous Thrombi Composition

A

Composed mainly of fibrin and trapped red blood cells with relatively few platelets

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7
Q

Atrial Thrombi Composition

A

Composed mainly of platelet aggregates held together by small amounts of fibrin

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8
Q

Anticoagulant Agent Uses

A

Drugs of choice for prevention and treatment of venous thromboembolism and for prevention of cardioembolic events in patients with atrial fibrillation. Anticoagulants are also effective for arterial thrombosis and their effects can be additive with antiplatelet agents

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9
Q

Antiplatelet Agent Uses

A

Drugs of choice primarily for prevention and treatment of arterial thrombosis (primary and secondary prevention and treatment of acute coronary syndrome).

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10
Q

Primary Prevention of ACS

A

W/ Risk Factors: Use Aspririn

W/O Risk Factors: Apsirin for Men >45 and women above >65

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11
Q

Secondary Prevention

A

Recent MI → Aspirin (clopidogrel if aspirin intolerant)

Ischemic Stroke → Aspirin + clopidogrel

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12
Q

UA/NSTEMI Treatment

A

Asprin
± clopidogrel
± UFH, LMWH or fondaparinux
± GPIIb/IIIa inhibitor

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13
Q

Acute MI (STEMI) Treatment

A

Aspirin + clopidogrel
+ UFH, LMWH or fondaparinux
+ GPIIb/IIIa inhibitor

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14
Q

PCI Treatment

A

Aspirin + clopidogrel
+ UFH, LMWH or fondaparinux
+ GPIIb/IIIa inhibitor

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15
Q

AFib Treatment

A

Warfarin or dabigatran or rivaroxaban or apixaban

(aspirin can be used for patients at low risk)

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16
Q

Venous Thromboembolism (VTE) Treatment

A

LMWH or UFH or

fondaparinux + warfarin

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17
Q

VTE Prevention

A

1) Hospitalized/Gen Surgery - Low-dose UFH or LMWH or fondaparinux
2) Ortho Surgery - Fondaparinux or rivaroxaban or dabigatran or LMWH or warfarin

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18
Q

PAD Treatment

A

Aspirin (clopidogrel if aspirin intolerant)

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19
Q

aPTT is used to monitor?

A

Heparin therapy (not significantly affected by LMWHs)

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20
Q

Heparin Mechanism

A

Binds to Antithrombin III (AT III) and increases its activity 1000 fold. Inhibits factors 2, 9, 10, 11, 12 and 13.

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21
Q

LMWH (Enoxapirin) and Fondaparinux Mechanisms

A
  • Bind to AT III and inactivate factor Xa, but not IIa (thrombin)
  • Claimed to have equal efficacy as regular heparin for VTE with less tendency for bleeding complications and less effects on platelets (i.e.,thrombocytopenia)
22
Q

Direct Thrombin IIa Inhibitors

A

Argatroban, bivalirudin, lepirudin, desirudin- all given parenterally

23
Q

Heparin & Derivative Pharmacokinetics

A

Not absorbed in GI Tract
Given Paranterally w/ IV Loading dose
Drug of choice if pregnant
FIRST ORDER RENAL ELIMINATION!!

24
Q

LMWH vs Heparin

A

LMWH Generally preferred due to less variable response (no monitoring needed) and less thrombocytopenia
Adjunct treatment in unstable angina/ acute MI

25
Q

Heparin/ Derivatives Adverse Rxns

A

Hemorrhage is the chief complication
Hypersensitivity
Thrombocytopenia
Osteoporosis

26
Q

Heparin & LMWH Overdosage Sign and Treatment

A

Bleeding is the chief sign

GIVE PROTAMINE!!

27
Q

Warfarin Mechanism

A

Acts in liver to prevent synthesis of clotting factors. Does not work until clotting factors are turned over.

28
Q

Warfarin Targets

A

Vitamin K-dependent clotting factors (II, VII, IX, X and Ca2+ dependent factors)

29
Q

Warfarin Uses

A

AFib

Prophylaxis/ treatment of thromboembolism

30
Q

Warfarin Adverse Rxns

A 
Hemorrhage
Necrosis of fatty soft tissue (use heparin bridge)
GI Issues
Osteoporosis
DON'T USE IF PREGNANT!
31
Q

Warfarin Overdose Signs and Treatments

A

Signs: Hematuria, excessive menorrhagia, gum bleeding

Major Bleeding- Hold warfarin, administer 5-10 mg of Vitamin K IV. Also use Prothrombin complex concentrate (PCC)

32
Q

Dabigatran Mechanism

A

Acts in the plasma to directly inhibit the activity of thrombin (Factor IIa). Does NOT require frequent monitoring and dosage adjustments. NO ANTIDOTE!

33
Q

Dabigatran Pharmacokinetic

A

Absorbed as a prodrug (etexilate) and converted to active form by plasma and liver esterases. Excreted renally.

34
Q

Dabigatran Uses

A

AFib!

35
Q

Dabigatran Adverse Rxns

A

Bleeding in 17% of pt’s (3% w/ major bleeding event)
GI Complaints
Fewer DDI than warfarin
Anticoagulant effect is IRREVERSIBLE!

36
Q

Antiplatelet Agents

A

Aspirin
Clopidogrel
Dipyridamole
Abciximab/ Eptifibatide/ Tirofiban

37
Q

Aspirin Mechanism

A

Small dose (40-80 mg) inhibits COX-1 synthesis of thromboxane in platelets. Largest [acetylsalicyclic acid] is in the portal vein so highest effect on circulating COX-1 (not tissue COX-2)

38
Q

Clopidogrel Mechanism

A

ADP (purinergic-P2Y12) receptor antagonists that interfere with ADP-induced platelet aggregation. Clopidogrel is prodrug converted to active metabolite by CYP450, which then irreversibly inhibits receptor.

39
Q

Dipyridamole Mechanism

A

Blocks phosphodiesterase breakdown of cAMP, elevating cAMP levels and potentiating prostacyclin’s anti-aggregatory action. Combined with aspirin as Aggrenox. Little or no apparent benefit as antithrombotic agent.

40
Q

Abciximab/Eptifibatide/Tirofiban Mechanism

A

Blocks IIb/IIIa receptors on platelet thus preventing integrin and fibrinogen binding that facilitates aggregation (platelet-platelet binding). Advantage of blocking all pathways of platelet activation.

41
Q

What antiplatelet agent(s) is/are dosed intravenously?

A

Abciximab, Eptifibatide, Tirofiban

42
Q

Clopidogrel Adverse Rxns

A

GI upset, headache, dizziness, upper respiratory infection, bleeding; concomitant use of proton pump inhibitors (PPIs) may inhibit activation of clopidogrel by CYP2C19

43
Q

Prasugrel and Ticagrelor Adverse Rxns

A

Bleeding!

44
Q

GIIb/IIIa inhibitor Adverse Rxns

A

Bleeding!

45
Q

Acute MI Anti-platelet drugs

A

Aspirin (chewed and swallowed) plus ADP antagonist

46
Q

Unstable Angina Anti-platelet drugs

A

Aspirin ± ADP antagonist

47
Q

Percutaneous Coronary Interventions (PCI) Anti-platelet drugs

A

Aspirin plus ADP antagonists ± GIIb/IIIa inhibitors

48
Q

Secondary Prevention of Acute MI Anti-platelet Drugs

A

Aspirin!

49
Q

Secondary Prevention of Ischemic Stroke Anti-platelet Drugs

A

Aspirin ± dipyridamole

50
Q

Anticoagulants we need to know

A

Heparin (UFH) / enoxaparin (LMWH), warfarin, dabigatran, rivaroxaban

51
Q

Antiplatelet agents we need to know

A

Aspirin, clopidrogel, GIIB/IIIa inhibitors (as class: abciximab / eptifibatide / tirofiban)

52
Q

Thrombolytic Agents we need to know

A

Tissue Plasminogen Activator (tPA) and variants

CVPR Unit 2 (15 decks)

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